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首页-抗体药物偶连体和PROTACs-PROTAC-BMS-986458
BMS-986458

Chemical Structure : BMS-986458

CAS No.: 3005272-36-3

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BMS-986458 (BMS986458)

货号: PC-24668Not For Human Use, Lab Use Only.

BMS-986458 is a potent, highly selective, orally bioavailable CRL4 CRBN E3 ubiquitin ligase-dependent BCL6 ligand directed degrader with CRBN binding IC50 of 41 nM, and BCL-6 degradation of 0.2 nM in OCI-LY-1 cells (2 h).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BMS-986458 is a potent, highly selective, orally bioavailable CRL4 CRBN E3 ubiquitin ligase-dependent BCL6 ligand directed degrader with CRBN binding IC50 of 41 nM, and BCL-6 degradation of 0.2 nM in OCI-LY-1 cells (2 h).
BMS-986458 demonstrates an exquisite selectivity for BCL6 degradation. In a panel of known CRBN neosubstrate assays, no degradation of CK1α, GSPT1, IKZF1, IZKF3, nor SALL4.
BMS-986458 potently exhibits antiproliferative effect against OCI-LY-1 cells with GI50 of 1.2 nM.
BMS-986458 rapidly degrades BCL6 protein to levels that drive broad anti-tumor effects in 80% of BCL6 expressing NHL cell lines and all ex vivo patient derived xenograft (PDX) models evaluated.

物理化学性质&存储条件

分子量 628.13
分子式 C32H34ClN9O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2,6-Piperidinedione, 3-[6-[[(3R,4R)-1-[5-chloro-4-[(2,3-dihydro-1-methyl-2-oxo-1H-indol-5-yl)amino]-2-pyrimidinyl]-3-methyl-4-piperidinyl]amino]-1-methyl-1H-indazol-3-yl]-

参考文献

1. Lynda Groocock, et al. Blood. Volume 144, Supplement 1, 5 November 2024, Page 957.

2. Patent WO2023212147 A1.

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